Cholesterol efflux capacity.

<p>Apolipoprotein B (apoB)-depleted sera of healthy subjects (control, n = 27) and patients with age-related macular degeneration (AMD, n = 29) were examined for (A) their ability to promote [³H]-cholesterol efflux from macrophages. [³H]-cholesterol-labeled RAW264.7 macrophages were incubated with 2.8% apoB-depleted sera for 4 hours. Cholesterol efflux is expressed as radioactivity in the supernatant relative to total radioactivity (in supernatant and cells). Values shown represent means of two independent experiments.</p

HDL-apolipoproteins and HDL associated lipids.

<p>Levels of total cholesterol (A), non-esterified cholesterol (FC) (B), phospholipids (PL) (C), free fatty acids (FFA) (D), triglycerides (TG) (E) were measured enzymatically in apoB depleted serum. HDL associated apolipoproteins ApoA-I (F), apoA-II (G), apoC-II (H), apoC-III (I) and apoE (J) were determined in apoB-depleted serum by immunoturbidimetry.</p

Paraoxonase activity.

<p>Activity of HDL-associated paraoxonase was measured using phenylacetate as substrate. Paraoxonase activity of apoB-depleted sera was calculated from the slopes of the kinetic chart. Values shown represent means of four independent experiments.</p

Anti-oxidative capability.

<p>The anti-oxidative activity of HDL was determined by inhibition of AAPH-initiated oxidation of the fluorescent dye dihydrorhodamine (DHR). Incubation of DHR in presence of apoB-depleted sera from healthy subjects or AMD patients led to a reduction in the oxidation of DHR. Values shown represent means of two independent experiments.</p

In vitro metabolic profile and in vivo antischistosomal activity studies of (η(6)-praziquantel)Cr(CO)3 derivatives

In vitro metabolic behavior was investigated for two chromium tricarbonyl derivatives of the antischistosomal drug praziquantel (PZQ) with the formula (η(6)-PZQ)Cr(CO)3 (1 and 2), by use of human liver microsomes. The metabolic profiles of the derivatives differ significantly. The optically pure (η(6)-PZQ)Cr(CO)3 derivatives (S, Sp)-1, (R, Rp)-1, (S, Rp)-2, and (R, Sp)-2 were also prepared to assess the eudysmic ratios of 1 and 2 against Schistosoma mansoni in vitro. A strong enantioselective antischistosomal activity was observed. The R-enantiomers are highly active against adult schistosomes in vitro (IC50 0.08-0.13 μM), whereas both S-enantiomers lack activity. The in vivo activity of 1 and 2 was then studied in mice harboring a chronic S. mansoni infection. A single dose of 1 and 2 (400 mg/kg) resulted in low worm burden reductions of 24% and 29% (p < 0.05)